EP2327699A4 - Glucocorticoid receptor agonist comprising novel 1,2,3,4-tetrahydroquinoxaline derivative containing phenyl group having sulfonic acid ester structure introduced therein as substituent - Google Patents
Glucocorticoid receptor agonist comprising novel 1,2,3,4-tetrahydroquinoxaline derivative containing phenyl group having sulfonic acid ester structure introduced therein as substituentInfo
- Publication number
- EP2327699A4 EP2327699A4 EP09813132A EP09813132A EP2327699A4 EP 2327699 A4 EP2327699 A4 EP 2327699A4 EP 09813132 A EP09813132 A EP 09813132A EP 09813132 A EP09813132 A EP 09813132A EP 2327699 A4 EP2327699 A4 EP 2327699A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- substituent
- novel
- acid ester
- sulfonic acid
- phenyl group
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
Links
- HORKYAIEVBUXGM-UHFFFAOYSA-N 1,2,3,4-tetrahydroquinoxaline Chemical class C1=CC=C2NCCNC2=C1 HORKYAIEVBUXGM-UHFFFAOYSA-N 0.000 title 1
- JFUAWXPBHXKZGA-IBGZPJMESA-N 4-fluoro-2-[(4r)-5,5,5-trifluoro-4-hydroxy-2-methyl-4-(1h-pyrrolo[2,3-c]pyridin-2-ylmethyl)pentan-2-yl]phenol Chemical compound C([C@@](O)(CC=1NC2=CN=CC=C2C=1)C(F)(F)F)C(C)(C)C1=CC(F)=CC=C1O JFUAWXPBHXKZGA-IBGZPJMESA-N 0.000 title 1
- 229940124750 glucocorticoid receptor agonist Drugs 0.000 title 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 title 1
- 125000002130 sulfonic acid ester group Chemical group 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
- C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
- C07D241/40—Benzopyrazines
- C07D241/42—Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
- C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
- C07D241/40—Benzopyrazines
- C07D241/44—Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Ophthalmology & Optometry (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2008234105 | 2008-09-12 | ||
PCT/JP2009/065888 WO2010029986A1 (en) | 2008-09-12 | 2009-09-11 | Glucocorticoid receptor agonist comprising novel 1,2,3,4-tetrahydroquinoxaline derivative containing phenyl group having sulfonic acid ester structure introduced therein as substituent |
Publications (2)
Publication Number | Publication Date |
---|---|
EP2327699A1 EP2327699A1 (en) | 2011-06-01 |
EP2327699A4 true EP2327699A4 (en) | 2011-12-28 |
Family
ID=42005236
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP09813132A Ceased EP2327699A4 (en) | 2008-09-12 | 2009-09-11 | Glucocorticoid receptor agonist comprising novel 1,2,3,4-tetrahydroquinoxaline derivative containing phenyl group having sulfonic acid ester structure introduced therein as substituent |
Country Status (12)
Country | Link |
---|---|
US (2) | US8664221B2 (en) |
EP (1) | EP2327699A4 (en) |
JP (1) | JP2010090117A (en) |
KR (1) | KR20110053467A (en) |
CN (1) | CN102149690A (en) |
AU (1) | AU2009292437A1 (en) |
BR (1) | BRPI0924571A2 (en) |
CA (1) | CA2735417A1 (en) |
EA (1) | EA018420B1 (en) |
GE (1) | GEP20135804B (en) |
MX (1) | MX2011002677A (en) |
WO (1) | WO2010029986A1 (en) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP5663934B2 (en) | 2010-04-09 | 2015-02-04 | ソニー株式会社 | Image processing apparatus, imaging apparatus, image processing method, and program |
CA2996278A1 (en) * | 2015-08-25 | 2017-03-02 | Santen Pharmaceutical Co., Ltd. | [4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1h-quinoxalin-7-yl)-phenoxy]ethyloxy compound or salt thereof |
SG10202007520WA (en) | 2016-03-02 | 2020-09-29 | Eisai R&D Man Co Ltd | Eribulin-based antibody-drug conjugates and methods of use |
CN110944668A (en) | 2017-06-16 | 2020-03-31 | 学校法人同志社 | Medicament comprising an mTOR inhibitor for treating or preventing ocular symptoms, disorders or diseases and uses thereof |
US20200121652A1 (en) | 2017-06-16 | 2020-04-23 | The Doshisha | Compounds having caspase inhibitory activity, pharmaceutical agent containing said compounds and for treating or preventing corneal endothelial symptoms, disorders, or diseases, and application of said pharmaceutical agent |
AR117951A1 (en) * | 2018-07-20 | 2021-09-08 | Gruenenthal Gmbh | TRIAZOLQUINOXALINE DERIVATIVES ADDITIONALLY SUBSTITUTED |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007105766A1 (en) * | 2006-03-14 | 2007-09-20 | Santen Pharmaceutical Co., Ltd. | Novel 1,2,3,4-tetrahydroquinoxaline derivative having glucocorticoid receptor binding activity |
WO2008146871A1 (en) * | 2007-05-29 | 2008-12-04 | Santen Pharmaceutical Co., Ltd. | Novel 1,2,3,4-tetrahydroquinoxaline derivative which has, as substituent, phenyl group having sulfonic acid ester structure or sulfonic acid amide structure introduced therein and has glucocorticoid receptor-binding activity |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6369057B1 (en) | 1991-04-15 | 2002-04-09 | Aventis Pharma Deutschland Gmbh | Quinoxalines, processes for their preparation and their use |
WO1997020578A1 (en) * | 1995-12-04 | 1997-06-12 | University Of Miami | Non-preserved topical corticosteroid for treatment of dry eye, filamentary keratitis, and delayed tear clearance |
US6340758B1 (en) | 1997-05-16 | 2002-01-22 | Warner-Lambert Company | Conformationally semi-constrained quinoxaline 2,3-diones as neuroprotective agents |
DE60113032T2 (en) | 2000-10-30 | 2006-07-06 | Pfizer Products Inc., Groton | Glucocorticoid receptor modulators |
JP2006525366A (en) | 2003-04-30 | 2006-11-09 | ジ インスチチュート フォー ファーマシューティカル ディスカバリー、エルエルシー | Heterocyclic carboxylic acid substituent |
US7235662B2 (en) | 2003-06-11 | 2007-06-26 | Bristol-Myers Squibb Company | Modulators of the glucocorticoid receptor and method |
EP1778242A4 (en) * | 2004-07-28 | 2010-10-20 | Irm Llc | Compounds and compositions as modulators of steroid hormone nuclear receptors |
CA2621292C (en) * | 2005-09-14 | 2014-05-27 | Santen Pharmaceutical Co., Ltd. | 1-2-dihydroquinoline derivative having glucocorticoid receptor binding actvity |
JP5054996B2 (en) | 2006-03-14 | 2012-10-24 | 参天製薬株式会社 | Novel 1,2,3,4-tetrahydroquinoxaline derivative having glucocorticoid receptor binding activity |
WO2007112347A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
US8008496B2 (en) | 2006-11-14 | 2011-08-30 | Santen Pharmaceutical Co., Ltd. | 1,2-dihydroquinoline derivative having substituted phenylchalcogeno lower alkyl group and ester-introduced phenyl group as substituents |
JP2008255112A (en) * | 2007-03-13 | 2008-10-23 | Santen Pharmaceut Co Ltd | Glucocorticoid receptor agonist composed of 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivative |
JP2009084274A (en) | 2007-09-13 | 2009-04-23 | Santen Pharmaceut Co Ltd | New 1,3,3-trimethyl-7-phenyl-3,4-dihydro-1h-quinoxalin-2-one derivative |
WO2009035067A1 (en) | 2007-09-13 | 2009-03-19 | Santen Pharmaceutical Co., Ltd. | Glucocorticoid receptor agonists consisting of 1,3,3-tri- methyl-7-phenyl-3,4-dihydro-1h-quinoxalin-2-one derivatives |
-
2009
- 2009-09-11 EA EA201100476A patent/EA018420B1/en not_active IP Right Cessation
- 2009-09-11 CN CN2009801357403A patent/CN102149690A/en active Pending
- 2009-09-11 CA CA2735417A patent/CA2735417A1/en not_active Abandoned
- 2009-09-11 US US13/063,186 patent/US8664221B2/en not_active Expired - Fee Related
- 2009-09-11 AU AU2009292437A patent/AU2009292437A1/en not_active Abandoned
- 2009-09-11 MX MX2011002677A patent/MX2011002677A/en unknown
- 2009-09-11 GE GEAP200912178A patent/GEP20135804B/en unknown
- 2009-09-11 EP EP09813132A patent/EP2327699A4/en not_active Ceased
- 2009-09-11 JP JP2009209876A patent/JP2010090117A/en active Pending
- 2009-09-11 KR KR1020117007506A patent/KR20110053467A/en not_active Application Discontinuation
- 2009-09-11 WO PCT/JP2009/065888 patent/WO2010029986A1/en active Application Filing
- 2009-09-11 BR BRPI0924571A patent/BRPI0924571A2/en not_active IP Right Cessation
-
2013
- 2013-10-22 US US14/059,817 patent/US20140045842A1/en not_active Abandoned
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007105766A1 (en) * | 2006-03-14 | 2007-09-20 | Santen Pharmaceutical Co., Ltd. | Novel 1,2,3,4-tetrahydroquinoxaline derivative having glucocorticoid receptor binding activity |
WO2008146871A1 (en) * | 2007-05-29 | 2008-12-04 | Santen Pharmaceutical Co., Ltd. | Novel 1,2,3,4-tetrahydroquinoxaline derivative which has, as substituent, phenyl group having sulfonic acid ester structure or sulfonic acid amide structure introduced therein and has glucocorticoid receptor-binding activity |
EP2151436A1 (en) * | 2007-05-29 | 2010-02-10 | Santen Pharmaceutical Co., Ltd | Novel 1,2,3,4-tetrahydroquinoxaline derivative which has, as substituent, phenyl group having sulfonic acid ester structure or sulfonic acid amide structure introduced therein and has glucocorticoid receptor-binding activity |
Non-Patent Citations (1)
Title |
---|
See also references of WO2010029986A1 * |
Also Published As
Publication number | Publication date |
---|---|
AU2009292437A1 (en) | 2010-03-18 |
EA201100476A1 (en) | 2011-10-31 |
KR20110053467A (en) | 2011-05-23 |
MX2011002677A (en) | 2011-04-12 |
US20110166151A1 (en) | 2011-07-07 |
JP2010090117A (en) | 2010-04-22 |
GEP20135804B (en) | 2013-04-10 |
CA2735417A1 (en) | 2010-03-18 |
US20140045842A1 (en) | 2014-02-13 |
US8664221B2 (en) | 2014-03-04 |
EP2327699A1 (en) | 2011-06-01 |
WO2010029986A1 (en) | 2010-03-18 |
CN102149690A (en) | 2011-08-10 |
EA018420B1 (en) | 2013-07-30 |
BRPI0924571A2 (en) | 2016-08-09 |
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Legal Events
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A4 | Supplementary search report drawn up and despatched |
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RIC1 | Information provided on ipc code assigned before grant |
Ipc: C07D 409/12 20060101ALI20111124BHEP Ipc: A61P 29/00 20060101ALI20111124BHEP Ipc: A61P 27/02 20060101ALI20111124BHEP Ipc: A61K 31/5377 20060101ALI20111124BHEP Ipc: A61K 31/498 20060101ALI20111124BHEP Ipc: C07D 241/44 20060101AFI20111124BHEP |
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